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A general and stereoselective method to synthesize 2,3,4,5,6-pentasubstituted tetrahydropyrans in three steps starting from three different aldehydes is described. Key substrates beta,gamma-unsaturated N-acyloxazolidin-2-ones were subjected to an “Evans Aldol-Prins” protocol to generate five sigma-bonds and five stereocenters in only a one-pot process with yields up to 60% and excellent stereoselectivities.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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The objective of the following study was to identify the source of high concentrations of glycol diethers (diglyme, triglyme, and tetraglyme) in the Oder River. Altogether four sampling campaigns were conducted and over 50 surface samples collected. During the first two samplings of the Oder River in the Oderbruch region (km 626-690), glymes were detected at concentrations reaching 0.065mugL-1 (diglyme), 0.54mugL-1 (triglyme) and 1.7mugL-1 (tetraglyme). The subsequent sampling of the Oder River, from the area close to the source to the Poland-Germany border (about 500km) helped to identify the possible area of the dominating glyme entry into the river between km 310 and km 331. During that sampling, the maximum concentration of triglyme was 0.46mugL-1 and tetraglyme 2.2mugL-1; diglyme was not detected. The final sampling focused on the previously identified area of glyme entry, as well as on tributaries of the Oder River. Samples from Czarna Woda stream and Kaczawa River contained even higher concentrations of diglyme, triglyme, and tetraglyme, reaching 5.2mugL-1, 13mugL-1 and 81mugL-1, respectively. Finally, three water samples were analyzed from a wastewater treatment plant receiving influents from a Copper Smelter and Refinery; diglyme, triglyme, and tetraglyme were present at a maximum concentration of 1700mugL-1, 13,000mugL-1, and 190,000mugL-1, respectively. Further research helped to identify the source of glymes in the wastewater. The gas desulfurization process Solinox uses a mixture of glymes (Genosorb1900) as a physical absorption medium to remove sulfur dioxide from off-gases from the power plant. The wastewater generated from the process and from the maintenance of the equipment is initially directed to the wastewater treatment plant where it undergoes mechanical and chemical treatment processes before being discharged to the tributaries of the Oder River. Although monoglyme was also analyzed, it was not detected in any of the water samples.

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Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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COMPOUND FOR INCREASING KINASE ACTIVE AND APPLICATION THEREOF

The compound of formula (I), pharmaceutically acceptable salts thereof, solvates thereof, chelates thereof, non-covalent complex thereof or produgs of compounds mentioned above or the mixture of any form above mentioned are provided. The use of the compounds in manufacturing a medicament for the treatment and/or prevention of diabetes, obesity and related disorders

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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A 4 – (2 – aminoethyl) tetrahydropyranylation synthetic method (by machine translation)

The invention belongs to the chemical pharmaceutical intermediates synthesis technology field, in particular to a pharmaceutical bei Fu citalopram intermediate 4 – (2 – aminoethyl) tetrahydropyranylation synthetic method. The method comprises the following steps: (1) 4 – chlorine four hydrogen pyranes with cyanoacetic acid methyl ester reaction to obtain the 2 – cyano – 2 – (tetrahydro – 4 – pyranyl) acetic acid methyl ester; (2) 2 – cyano – 2 – (tetrahydro – 4 – pyranyl) methyl acetate obtained with protective cover (tetrahydro – 4 – pyranyl) – b nitriles; (3) (tetrahydro – 4 – pyranyl) – b nitrile C hydrogenation reaction to obtain 4 – (2 – aminoethyl) tetrahydropyran. The method adopts the 4 – chlorine four hydrogen pyranes, cyanoacetic acid methyl ester as the raw material, the method has short reaction time, low cost, easily available raw materials, non-toxic control and not stable chemical raw materials, safe and effective, the yield is high, less impurities. (by machine translation)

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Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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PYRAZOLE COMPOUNDS AS JAK INHIBITORS

The present invention relates to compounds of formula (I), wherein R1, R2, R1a, R1b have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Suzuki cross-coupling reactions of an unprecedented array of unactivated primary and secondary alkyl halides (including challenging alkyl chlorides) can be accomplished through the use of nickel/amino alcohol-based catalysts. Both the nickel precatalyst and the amino alcohols (prolinol or trans-2-aminocyclohexanol) are commercially available and air-stable. In view of the remarkable diversity of amino alcohols that are readily accessible, this discovery may open the door to the rapid development of versatile catalysts for a wide range of cross-coupling processes. Copyright

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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The dipole moments of some 3- and 4-bromo and chloro heteracyclohexanes are measured by the method of Debye and calculated both by the quantum-mechanical method CNDO/2 and vector addition method.The determination of conformational free energy is made on the basis of measured dipole moments mu of the conformation mixture and the calculated dipole moments mue and mua of the pure conformers.The results are discussed in relation to n.m.r.-results.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R2, R3, R4, R5, and and R6 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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4-Cyclohexylbutyl-N-[(S)-2-oxoazetidin-3-yl]carbamate (3b) is a potent, selective and systemically active inhibitor of intracellular NAAA activity, which produces profound anti-inflammatory effects in animal models. In the present work, we describe structure-activity relationship (SAR) studies on 3-aminoazetidin-2-one derivatives, which have led to the identification of 3b, and expand these studies to elucidate the principal structural and stereochemical features needed to achieve effective NAAA inhibition. Investigations on the influence of the substitution at the beta-position of the 2-oxo-3-azetidinyl ring as well as on the effect of size and shape of the carbamic acid ester side chain led to the discovery of 3ak, a novel inhibitor of human NAAA that shows an improved physicochemical and drug-like profile relative to 3b. This favourable profile, along with the structural diversity of the carbamic acid chain of 3b, identify this compound as a promising new tool to investigate the potential of NAAA inhibitors as therapeutic agents for the treatment of pain and inflammation.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Alkyl-alkyl Suzuki cross-coupling of unactivated secondary alkyl chlorides

No such thing as a problem substrate! In a reaction designed specifically for the title substrates C-C coupling with alkyl boranes occurred in good yield at room temperature with commercially available catalyst components (see scheme). This versatile method is also suitable for Suzuki reactions of secondary and primary alkyl bromides and iodides, as well as primary alkyl chlorides.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics